通过直接将脂质体悬浮液注入液相色谱法，可以简便，快速地测定负载阿霉素的脂质体的包封效率。,International Journal of Pharmaceutics

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通过直接将脂质体悬浮液注入液相色谱法，可以简便，快速地测定负载阿霉素的脂质体的包封效率。
International Journal of Pharmaceutics ( IF 5.3 ) Pub Date : 2017-11-28 , DOI: 10.1016/j.ijpharm.2017.11.035
Eiichi Yamamoto ₁ , Shota Miyazaki ₂ , Chiaki Aoyama ₂ , Masaru Kato ₃

Affiliation

开发了一种简单快速的色谱测量方法，用于使用纳米颗粒排阻色谱法（nPEC）确定将阿霉素（DOX）包封到聚乙二醇化脂质体中的效率（EE）。在这项工作中，将Doxil®和掺有DOX的两个PEG化脂质体用作模型脂质体，并使用N-乙烯基吡咯烷酮修饰的nPEC色谱柱通过二极管阵列检测器通过高效液相色谱法对未封装的DOX进行了测量，而无需任何样品预处理。只需5μL完整的脂质体悬浮液和3分钟的分析时间即可确定未封装的DOX的量。方法的线性，准确性，精密度和回收率均在0.00-1.0 mg / mL（相当于100-50％EE）的范围内进行了验证。该方法的适用性是通过使用硫酸铵梯度的远程加载方法测量时间依赖性DOX加载到脂质体中的百分比来确认的。此外，发现色谱图中负载DOX的脂质体的峰面积与DOX EE％成正比。由于这种简单，快速的分析方法可以精确地测量EE，因此有望将该方法应用于脂质体制剂生产的过程控制和脂质体药物产品的质量控制。

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A simple and rapid measurement method of encapsulation efficiency of doxorubicin loaded liposomes by direct injection of the liposomal suspension to liquid chromatography.

A simple and rapid chromatographic measurement method for determining doxorubicin (DOX) encapsulation efficiency (EE) into PEGylated liposomes using nanoparticle exclusion chromatography (nPEC) was developed. In this work, Doxil® and two PEGylated liposomes spiked with DOX were employed as model liposomes, and unencapsulated DOX was measured by high performance liquid chromatography with diode-array detector using an N-vinylpyrrolidone modified nPEC column without any sample pretreatment. Only 5 μL of an intact liposomal suspension and 3 min analysis time were required for the determination of the quantity of unencapsulated DOX. The method was validated in terms of linearity, accuracy, precision, and recovery in the range from 0.00-1.0 mg/mL (corresponding to 100-50% EE). Applicability of the method was confirmed using the measurement of time-dependent DOX loading% into the liposomes with the remote loading method using an ammonium sulfate gradient. Furthermore, it was found that the peak area of DOX-loaded liposomes in the chromatogram was proportional to DOX EE%. As this simple and rapid analytical method can measure the EE precisely, it is expected that this method will be applicable to the in-process control of liposome preparation manufacturing and the quality control of the liposome drug products.

更新日期：2019-11-01

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